Antihyperglycemic activity of 2-methyl-3,4,5-triaryl-1 H -pyrroles in SLM and STZ models

Goel, Atul; Agarwal, Nidhi; Singh, Fateh V.; Sharon, Ashoke; Tiwari, Piyush; Dixit, Manish; Pratap, Ramendra; Srivastava, Arvind K.; Maulik, Prakas R.; Ram, Vishnu Ji

doi:10.1016/j.bmcl.2004.01.009

Cited by 88 publications

(37 citation statements)

References 15 publications

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“…In fact, it is the starting material for the synthesis of 2,3,5-substituted tetrahydrofurans (cancer chemopreventives [12] and selective COX-Z inhibitors [13] ) of 4,5-diarylimidaxoles (human CB1 receptor inverse agonists), [14] of 3,4,5-triaryl-1H-pyrroles (antihyperglycemic molecules), [15] etc. Moreover, some substituted benzoins have themselves pharmacological activities.…”

Section: Introductionmentioning

confidence: 99%

Study on the Reactivity of Aldehydes in Electrolyzed Ionic Liquids: Benzoin Condensation – Volatile Organic Compounds (VOCs) vs. Room Temperature Ionic Liquids (RTILs)

et al. 2010

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The benzoin condensation of aromatic and heteroaromatic aldehydes, catalyzed by electrochemically generated N-heterocyclic carbenes, has been set up in the absence of organic solvents and bases. a-Hydroxy ketones have been isolated in good to elevated yields, in short reaction times. Aldol products and carbene-aldehyde adducts have been obtained in elevated yields from linear and short branched aldehydes, respectively. A comparison with the use of classical organic solvents has been reporte

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Section: Introductionmentioning

confidence: 99%

Study on the Reactivity of Aldehydes in Electrolyzed Ionic Liquids: Benzoin Condensation – Volatile Organic Compounds (VOCs) vs. Room Temperature Ionic Liquids (RTILs)

et al. 2010

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“…The present study demonstrated increased Na + excretion, and improved renal function as indicated by reduction in serum creatinine levels with individual treatments. This renal improvement accompanied with increased Na + excretion may be one of the factors responsible for reduction in BP in diabetic rats [19,32]. It is well known that the Zucker fa/fa rats have abnormal renal function.…”

Section: Discussionmentioning

confidence: 99%

Effect of combination treatment of S–amlodipine with peroxisome proliferator-activated receptor agonists on metabolic and cardiovascular parameters in Zucker fa/fa rats

Singh

Sangle

Murugan

et al. 2014

Diabetol Metab Syndr

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BackgroundType 2 diabetes is a complex metabolic disorder characterized by hyperglycemia, impaired glucose tolerance and insulin resistance associated with dyslipidemia and hypertension. The available drugs are not sufficiently efficacious in reducing cardiovascular risk and restoring normal glucose metabolism associated with type 2 diabetes as a mono- or a combination therapy. The present study examined the combined effects of an antihypertensive (S-Amlodipine) and an insulin-sensitizing agent, peroxisome proliferator-activated receptor (PPAR) agonists (Pioglitazone and Ragaglitazar), on cardiovascular risk factors in aged diabetic and insulin-resistant Zucker fa/fa rats.MethodsFollowing combination treatment for 14 days, blood pressure (BP), serum glucose, total cholesterol and triglycerides were measured. Aortic ring study was conducted to determine the effect of combination treatments on phenylephrine-induced vasoconstriction and acetylcholine (Ach)-induced vasorelaxation.ResultsIn combination, S-Amlodipine and Pioglitazone significantly reduced blood glucose (115.1 ± 6.6 vs. 81.7 ± 4.2), BP (184.4 ± 5.0 vs. 155.1 ± 5.0), serum triglycerides (362.5 ± 47.5 vs. 211.1 ± 23.7) and glucose intolerance when compared with vehicle treated Zucker fa/fa rats. Similar results were observed with the combination of S-Amlodipine and Ragaglitazar (Triglycerides, 362.5 ± 47.5 vs. 252.34 ± 27.86; BP, 184.4 ± 5.0 vs. 159.0 ± 8.0) except for serum glucose. ACh-induced vasorelaxation in aortic rings was also superior with both of the combinations compared to individual treatment. Furthermore, there was less body weight gain and food intake with S-Amlodipine and Pioglitazone combination in Zucker fa/fa rats. S-Amlodipine itself caused significant reduction in glucose (115.1 ± 6.6 vs. 89.7 ± 2.7) and BP (184.4 ± 5.0 vs. 156.1 ± 4.0) with improvement in insulin sensitivity observed through oral glucose tolerance test.ConclusionsThe results suggest that a combination of PPAR agonists and S-Amlodipine has partial benefits in improving the cardiovascular risk factors such as reduction in triglyceride levels, associated with chronic type 2 diabetes, and therefore may be utilized as an approach for addressing some of these devastating metabolic syndrome complications.

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“…(a) Pyrroles as antihyperglycemic agents [19, 20], (b) Amaryl, standard antihyperglycemic drug [21, 22], and approved DPP-IV inhibitors [23–25] as type 2 diabetes medications containing a pyrrole moiety. (c) Thieno and Pyrrolo-pyrimidines as DPP-IV inhibitors.…”

Section: Figurementioning

confidence: 99%

“…For several decades, interest in pyrrole derivatives increases due to their pharmaceutical importance [1–3], such as antimicrobial [4–8], antiviral [9, 10], anti-inflammatory [11–13], analgesic [14], antitumor [15, 16], antihyperlipidemic [17], anticonvulsant [18], and antihyperglycemic agents [19, 20], as shown in Figures 1 and 2(a).…”

Section: Introductionmentioning

confidence: 99%

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Synthesis and Evaluation of Novel Pyrroles and Pyrrolopyrimidines as Anti-Hyperglycemic Agents

Mohamed

Ali

Abdelaziz

et al. 2014

BioMed Research International

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A series of pyrrole and pyrrolopyrimidine derivatives were examined for their in vivo antihyperglycemic activity. Compounds Ia–c,e, and IVg showed promising antihyperglycemic activity equivalent to a well-known standard antihyperglycemic drug, Glimepiride (Amaryl, 4 mg/kg). In this paper, we examine and discuss the structure-activity relationships and antihyperglycemic activity of these compounds.

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Antihyperglycemic activity of 2-methyl-3,4,5-triaryl-1 H -pyrroles in SLM and STZ models

Cited by 88 publications

References 15 publications

Study on the Reactivity of Aldehydes in Electrolyzed Ionic Liquids: Benzoin Condensation – Volatile Organic Compounds (VOCs) vs. Room Temperature Ionic Liquids (RTILs)

Study on the Reactivity of Aldehydes in Electrolyzed Ionic Liquids: Benzoin Condensation – Volatile Organic Compounds (VOCs) vs. Room Temperature Ionic Liquids (RTILs)

Effect of combination treatment of S–amlodipine with peroxisome proliferator-activated receptor agonists on metabolic and cardiovascular parameters in Zucker fa/fa rats

Synthesis and Evaluation of Novel Pyrroles and Pyrrolopyrimidines as Anti-Hyperglycemic Agents

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